Cabazitaxel was developed by Sanofi-Aventis and was approved by FDA in 2010. JEVTANA® (cabazitaxel) is a microtubule inhibitor indicated in combination with prednisone for the treatment of patients with hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen.
Cabazitaxel is an anti-neoplastic agent belonging to the taxane class. It is prepared by semi-synthesis with a precursor extracted from yew needles. The chemical name of cabazitaxel is (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[(tertbutoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate-propan-2-one(1:1). Its chemical structure is shown below.

Cabazitaxel is a white to off-white powder with a molecular weight of 894.01 (for the acetone solvate)/835.93 (for solvent free). Cabazitaxel is known to have poor solubility in water or general pharmaceutical solvents. It is lipophilic, soluble in alcohol, but practically insoluble in water. JEVTANA® (cabazitaxel) Injection (60 mg/1.5 mL) is a sterile, non-pyrogenic, clear yellow to brownish-yellow viscous solution and is available in a single-use vial containing 60 mg cabazitaxel (anhydrous and solvent free) and 1.56 g polysorbate 80. Each mL contains 40 mg cabazitaxel (anhydrous) and 1.04 g polysorbate 80. JEVTANA® Injection requires two dilutions prior to administration.
Diluent for JEVTANA® is a clear, colorless, sterile, and non-pyrogenic solution containing 13% (w/w) ethanol in water for injection, approximately 5.7 mL. JEVTANA® Injection is first diluted with a supplied Diluent for JEVTANA®, followed by a second dilution in either 0.9% sodium chloride solution or 5% dextrose solution for administering to a patient. First diluted solution of JEVTANA® should be used immediately (within 30 minutes) for preparing the second diluted injectable solution. Both JEVTANA® Injection and Diluent should be stored at 25° C. (permitted between 15-30° C.), and should not be refrigerated.
The complexity of preparing two dilutions of a cabazitaxel injection solution for use is inconvenient and increases the risk of bacteria infection.
There is a need for a single-vial and stable formulation for cabazitaxel, which can be diluted once for intravenous infusion.